Brazilian Journal of Pharmaceutical Sciences, Volume: 54, Issue: 3, Published: 2018
  • Hair straighteners: an approach based on science and consumer profile Review

    Leite, Marcella Gabarra Almeida; Garbossa, Wanessa Almeida Ciancaglio; Campos, Patricia Maria Berardo Gonçalves Maia

    Abstract in English:

    Technological progress has allowed women to change their natural hair configuration according to their will. This type of treatment is very popular around the world, even involving the use of prohibited chemicals, such as formaldehyde. Studies of hair characterization, straighteners and toxic evaluation are available in the literature, although few studies have evaluated the consumer profile or the current legislation of Brazil and the European Union (EU) and its influence on the consumption of hair straighteners. Previous studies from our research group have shown that hair care is essential for the quality of life and well-being of women. Within this context, the present study aimed to evaluate the profile of Brazilian hair straightener consumers, as well as the legislation of Brazil and the EU and its influence on the use of these products. The consumer profile was evaluated by applying questionnaires and the legislation was examined using documental and bibliographic exploratory research. The results provided a full understanding of the current legislation of Brazil and its similarities to EU legislation. It was observed that over 50% of Brazilians currently use or have previously used hair straightener products, even persons who do not have curly hair, suggesting that straight hair is more attractive for today’s society. Although the study participants consider the current legislation to be important, over 40% do not know the active ingredients present in the hair straightener they use. Finally, the legislation is not considered in terms of the daily hair treatment routine, with the esthetic result being more important to the consumer.
  • Studies on new substituted pyridazinones: synthesis and biological evaluation Article

    Asif, Mohammad; Singh, Anita; Khan, Shah Alam; Husain, Asif

    Abstract in English:

    We report herein the synthesis and pharmacological evaluation of a new series of 6-aryl-2-(imidazol-1-yl/1,2,4-triazol-1-yl)-2-methyl-4,5-dihydro-(2H)-pyridazin-3-one (3a-j) as potential anticonvulsant and antitubercular agents. The title compounds were prepared by reacting 6-aryl-4,5-dihydro-(2H)-pyridazin-3-one (2a-e) with formaldehyde and secondary cyclic amine imidazole or 1,2,4-triazole as per Mannich reaction. Anticonvulsant activity of pyridazinone derivatives was tested at 50 mg.kg-1 dose level against maximal electroshock (MES), isoniazid (INH, 250 mg.kg-1) and pentylenetetrazole (PTZ at 80 mg.kg-1) induced seizure methods. Phenytoin sodium (25 mg.kg-1) and sodium valproate (100 mg.kg-1) were used as reference drugs for comparison purpose. In-vitro antitubercular activity was tested by Microplate Alamar Blue assay (MABA) method and the results were compared with clinically used antitubercular agents such as INH, Pyrazinamide (PZA) and Streptomycin (STM). None of the screened compounds were found to be neurotoxic at a dose level of 100 mg.kg-1. All the screened compounds (3a-j) significantly reduced the MES, INH and PTZ induced convulsions and thus showed good anticonvulsant activity. The minimum inhibitory concentration (MIC) of the title compounds against M. tuberculosis ranged from 1.6 µg/mL to 6.25 µg/mL in comparison to INH, PZA (3.125 µg/mL) and STM (6.25 µg/mL) which indicated good antitubercular activity.
  • Ability of two new thiazolidinediones to downregulate proinflammatory cytokines in peripheral blood mononuclear cells from children with asthma Article

    Rêgo, Moacyr Jesus Barreto de Melo; Azoubel-Antunes, Adriana; Bezerra, Mariana Brayner-Cavalcanti Freire; Pereira, Michelly Cristiny; Silva, Juliana Cruz da; Lins, Thiago Ubiratan Lins e; Sarinho, Emanuel Sávio Cavalcanti; Amorim, Cézar Augusto da Cruz; Lima, Maria do Carmo Alves de; Galdino-Pitta, Marina Rocha; Pitta, Ivan da Rocha; Pitta, Maira Galdino da Rocha

    Abstract in English:

    Allergic asthma is a chronic, complex inflammatory disease of the airway. Despite extensive studies on the immunomodulation of T helper (Th) cell pathways (i.e., Th1 and Th2) in asthma, little is known about the effects of Th17 pathway modulation, particularly that involving peroxisome proliferator-activated receptors (PPARs). In response, two new thiazolidinedione derivatives-namely, LPSF-GQ-147 and LPSF-CR-35 were synthesized and evaluated for their immunomodulatory effects on Th17-related cytokines, including interferon γ (IFNγ), interleukin IL-6, IL-17, and IL-22 in the peripheral blood mononuclear cells of asthmatic children. Both compounds were nontoxic even at high concentrations (i.e., 100 µM). The LPSF-CR-35 compound significantly reduced the levels of IL-17A (p = .039) and IFNγ (p = .032) at 10 µM. For IL-22 and IL-6, significant reduction occurred at 100 µM (p = .039 and p = .02, respectively). Conversely, LPSF-GQ-147 did not significantly inhibit the production of the tested cytokines, the levels of all of which were more efficiently reduced by LPSF-CR-35 than methylprednisolone, the standard compound. Real-time polymerase chain reaction assay confirmed that LPSF-GQ-147 has significant PPARγ modulatory activity. Such data indicate that both LPSF-CR-35 and LPSF-GQ-147 are promising candidates as drugs for treating inflammation and asthma.
  • Forced degradation of gliquidone and development of validated stability-indicating HPLC and TLC methods Article

    El-ghobashy, Mohamed Refaat; Yehia, Ali Mohamed; Helmy, Aya Helmy; Youssef, Nadia Fayek

    Abstract in English:

    Forced degradation studies of gliquidone were conducted under different stress conditions. Three degradates were observed upon using HPLC and TLC and elucidated by LC-MS and IR. HPLC method was performed on C18 column using methanol-water (85:15 v/v) pH 3.5 as a mobile phase with isocratic mode at 1 mL.min-1 and detection at 225 nm. HPLC analysis was applied in range of 0.5-20 µg.mL-1 (r =1) with limit of detection (LOD) 0.177 µg.mL-1. TLC method was based on the separation of gliquidone from degradation products on silica gel TLC F254 plates using chloroform-cyclohexane-glacial acetic acid (6:3:1v/v) as a developing system with relative retardation 1.15±0.01. Densitometric measurements were achieved in range of 2 -20 µg /band at 254 nm (r = 0.9999) with LOD of 0.26 µg /band. Least squares regression analysis was applied to provide mathematical estimates of the degree of linearity. The analysis revealed a linear calibration for HPLC where a binomial relationship for TLC. Stability testing and methods validation have been evaluated according to International Conference on Harmonization guidelines. Moreover, the proposed methods were applied for the analysis of tablets and the results obtained were statistically compared with those of pharmacopeial method revealing no significant difference about accuracy and precision.
  • Pharmaceutical clinical services in basic care in a region of the municipality of São Paulo Article

    Santos, Felipe Tadeu Carvalho; Silva, Dayde Lane Mendonça da; Tavares, Noemia Urruth Leão

    Abstract in English:

    Pharmaceutical care has undergone several transformations in the health context over the years. Thus, the pharmacist has suffered a reconfiguration of his performance, mainly with the incorporation of clinical services and patient approach. The study analyzed the results of the implementation of pharmaceutical clinical services in Primary Health Care, through the use of indicators of supply, demand and productivity, clinical and process quality related to pharmaceutical care. We included all the clinical visits (n=1,833) performed to 1,080 users in 12 Basic Health Unit facilities from May to November 2016, of which 40.8% (n=748) were consultations in the establishments and 50.2% (n=1,085) home visits. Most patients (73.5%) were referred by team and 17.5% were captured through active search. Of the total workload, 12.5% ​​were dedicated to pharmaceutical consultations and 20.0% to home visits. In total, we identified 3,078 pharmacotherapy-related issues, an average of 2.8 per patient, and 6,882 pharmaceutical interventions were performed, equivalent to 6.3 interventions per patient. The problem with adherence to pharmacotherapy and the intervention of medication counseling were the most found. Results reinforce the importance of pharmaceutical clinical services in identifying the control of the most prevalent health conditions and monitoring the therapeutic results associated with drug use.
  • Synthesis and in vitro anti-HIV-1 evaluation of some N-arylsulfonyl-3-formylindoles Article

    Che, Zhiping; Tian, Yuee; Liu, Shengming; Hu, Mei; Chen, Genqiang

    Abstract in English:

    As our ongoing work on research of anti-HIV-1 inhibitors, fifteen N-arylsulfonyl-3-formylindoles (3a-o) were designed and prepared through two step synthetic route. Firstly, 3-formylindoles (2a-c) were synthesized via the Vilsmeier-Haack reaction. Subsequently, treatment of 2a-c with the appropriate arylsulfonyl chlorides led to the corresponding target compounds in excellent yields. All analogues were also preliminary evaluated in vitro for their inhibitory activity against HIV-1 replication. Among of all the reported analogues, three compounds 3c, 3g and 3i displayed significant anti-HIV-1 activity, with EC50 values of 9.57, 11.04 and 5.02 μM, and TI values of 31.89, 13.79 and 81.69, respectively. N-m-nitrophenylsulfonyl-3-formylindole (3c) and N-m-nitrophenylsulfonyl-6-methyl-3-formylindole (3i) especially exhibited the best promising anti-HIV-1 activity. In addition, it demonstrated that insertion of a methyl group at the C-6 position of the indolyl ring and a nitro group at the meta position of the arylsulfonyl ring, as in compound 3i, resulted in both low cytotoxicity (CC50= 410.41 μM) and good antiviral activity.
  • A study of the phytotoxic effects of the aerial parts of Senecio westermanii Dusén (Asteraceae) on Lactuca sativa L. and Allium cepa L. seeds Article

    Merino, Francis José Zortéa; Ribas, Daniele Felipe; Silva, Cristiane Bezerra da; Duarte, Ana Flávia Schvabe; Paula, Cristiane da Silva; Oliveira, Maislian de; Dias, Josiane de Fátima Gaspari; Miguel, Marilis Dallarmi; Miguel, Obdulio Gomes

    Abstract in English:

    The objective of this study was to evaluate the effects of the ethanolic crude extracts and fractions of the species Senecio westermanii Dusén on Lactuca sativa L. (lettuce) and Allium cepa L. (onion) seeds. We assessed the germination, growth, root respiration and photosynthesis of the target species in Petri dishes (9.0 cm diameter) containing filter paper n°6. The study was conducted using 50 seeds per plate and held in 4 replicates per concentration of each sample. In the germination there was an inhibitory effect of fractions hexane (FH) and chloroform (FCl) at concentrations of 500 and 1000 µg/mL. There was a reduction in the radicle growth of lettuce by 14 to 24% and a reduction of hypocotilum by 14 to 28%. As for the radicle of the onion was up 74% reduction to the FCl and the coleoptile was 24 and 45% reduction for FH and FCl, respectively. Inhibitory effects in the root respiration of lettuce were detected in all the samples analyzed, with results ranging from 16 to 83%. For the seeds of A. cepa, there was an encouragement for the FCl and ethyl acetate fractions (FAE), with results ranging from 94 to 142% and 76 to 150%, respectively. With regard to the photosynthesis of L. sativa, there was no significant difference between the control, and as for the A. cepa, there was a strain in inhibition concentrations of 250 and 500 µg/mL, which ranged from 27 to 68%. The samples of S. westermanii caused changes in the target species and thus can be used as a natural herbicide.
  • Stability indicating RP-HPLC method development and validation of cefepime and amikacin in pure and pharmaceutical dosage forms Article

    Kalyani, Lella; Rao, Chava Venkata Nageswara

    Abstract in English:

    A simple, accurate, isocratic stability indicating RP-HPLC method was developed for the determination of cefepime and amikacin in Pure and its pharmaceutical formulations. The method consists of methanol: acetonitrile:acetate buffer 75:20:05 (v/v) mobile phase at pH 5.1 with C18 column as stationary phase. The flow rate and detection wave length were 1.0 mL/min and 212 nm respectively. The linearity range for the method was found to be 2.5-25 µg/mL for amikacin and 10-100 µg/mL cefepime respectively. The developed method was validated as per ICH guidelines and the results of all the validation parameters were well within their acceptance values. Also the forced degradation studies were conducted with standard drugs. Degradation products formed during the different stress conditions were separated from both drugs. This validated method was applied for the simultaneous estimation of cefepime and amikacin in commercially available formulation sample.
  • 6 weeks consumption of pure fresh coconut milk caused up-regulation of eNOS and CSE protein expression in middle-aged male rats Article

    Jansakul, Chaweewan; Naphatthalung, Jomkarn; Pradab, Sakda; Yorsin, Somruedee; Kanokwiroon, Kanyanatt

    Abstract in English:

    Coconut milk (CCM) has been an important cooking ingredient in the Asia-Pacific region since ancient time. Due to its high content of saturated fatty acids, it has been considered atherogenic. We have tested if chronic consumption of fresh coconut milk by middle-aged male rat affects vascular function, plasma glucose and lipid profiles. Compared to control, CCM caused lower maximal contraction to phenylephrine of thoracic aortic rings and increased relaxation to acetylcholine that was abolished by N G-nitro-L-arginine (L-NA) or disruption of the endothelium. DL-propargylglycine caused slight increase in baseline tension of L-NA treated aortic rings of CCM-treated rats and produced higher contractile response of the aortic rings to low concentrations of phenylephrine. The aortic eNOS- and cystathionine-γ-lyase(CSE) proteins expression of the CCM-treated rats were also higher than in controls. Except for lower fasting plasma glucose there were no changes in blood chemistry for the CCM treated rats. CCM consumption caused up-regulation of eNOS and CSE protein expression which resulted in increased production of NO and H2S from the blood vessels with attenuation of vasocontraction to phenylephrine and increased relaxation to acetylcholine. These novel benefits may be expected to reduce the development of cardiovascular risk factors in the aging rat.
  • Preparation and in vitro & in vivo evaluation of cephalexin matrix tablets Article

    Reddy, Boi Basanta Kumar; Nagoji, Kambhayathughar Eswara Venkata; Sahoo, Satyanarayan

    Abstract in English:

    The purpose of the study is to develop cephalexin controlled-release matrix tablets by using lower proportions of release retardant polymer and to establish their in vitro & in vivo correlation. Tablets were compressed by incorporating polymers in a matrix form along with drug which prolong the drug release. Twelve formulations were prepared by mixing ethyl cellulose (EC) and hydroxypropyl methylcellulose (HPMC) (three different viscosity grades) in various proportions. F-1 to F-4 formulations were prepared by incorporating drug, HPMC K4M and ethyl cellulose in 100 : 5 : 5, 100 : 10 : 5, 100 : 15 : 5 and 100 : 20 : 5; similarly, F-5 to F-8 were prepared with HPMC K15M; and F-9 to F-12 were prepared with HPMC K100M using a wet granulation process maintained same proportions, along with drug and EC. Tablets were evaluated for their pre-compression and post-compression characteristics and they were found to be in limits. From the dissolution testing, F-4 showed 100.34% medicament release in 12 h. In vivo studies were conducted on rabbit and pharmacokinetic parameters of the optimized formulation were evaluated using HPLC method. It was found that matrix tablets showed increased t1/2 and decreased Kel. The design signified that the drug release rate from tablets was influenced by the small proportion (around 7% of a tablet weight) of polymer mixture and it controlled 100% medicament release upto 12 h effectively with the low grade viscosity of HPMC combination, with good in vitro & in vivo correlation.
  • Synthesis of leading chalcones with high antiparasitic, against Hymenolepis nana, and antioxidant activities Article

    Díaz-Carrillo, José Tomás; Díaz-Camacho, Sylvia Páz; Delgado-Vargas, Francisco; Rivero, Ignacio Alfredo; López-Angulo, Gabriela; Sarmiento-Sánchez, Juan Ignacio; Montes-Avila, Julio

    Abstract in English:

    The hymenolepiosis by Hymenolepis nana is a major public health problem in developing countries, and the commercial drugs against this parasitosis are not enough effective. The combination of antiparasitic and antioxidant agents has improved the treatment of some parasitoses. Thus, the development of new cestocidal and antioxidant agents to treat the hymenolepiosis cases is important. In the present study, four hydroxy- and four dihydroxy-chalcones were synthesized using the catalyst boron trifluoride diethyl etherate (BF3•OEt2). The antioxidant activity and antiparasitic against H. nana of chalcones were tested, as well as the toxicity by the brine shrimp lethality bioassay and the method of Lorke. The antioxidant activity was measured by three radical scavenging assays: 2,2’-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing antioxidant power (FRAP). The hydroxyl substitution pattern (number and position), mainly in ring B, was responsible for the chalcone antiparasitic activity. At least one meta or para hydroxyl group in ring B was essential for activity of the synthetic chalcones against H. nana; The time taken for the parasite to die by the 3b and 3e chalcones (20 mg/mL) treatment was up to six times lower than the control drug Praziquantel. On the other hand, chalcones with catechol structure in ring B (3g and 3h) showed the highest antioxidant values. The toxicity evaluations suggests that synthetic hydroxychalcones with cestocidal (3b and 3e) and antioxidant (3g and 3h) activities are safe compounds and potential in vivo agents to treat this parasitosis.
  • A smart approach for delivery of aripiprazole via oro-soft palatal mucosal route for improved therapeutic efficacy Article

    Madhav, Nookala Venkala Satheesh; Ojha, Abhijeet; Jaiswal, Vishakha

    Abstract in English:

    Effective management of schizophrenia, acute mania, mixed episodes associated with bipolar disorders, and depression can be managed with aripiprazole moiety. In the present research work an attempt was made to minimize the dose related side effects thus improving the quality life of the patients. A novel biopolymer was isolated from the fruits of Trachyspermum ammi. Ten optimized nanosized aripiprazole loaded formulations were prepared in 1-5% concentration of biopolymer (FA1-FA5) and sodium CMC (FM1-FM5) by solvent casting technique. The formulated flexy films were evaluated for thickness, folding endurance, weight uniformity, surface pH, mucoadhesivity, In-vitro drug release studies, In-vivo pharmacodynamic study and stability studies. The isolated biopolymer showed inbuilt fimability and mucoadhesivity and consists of carbonyl, hydroxyl and thiocarbonyl functional groups. All formulations showed folding endurance from 153 to 170, mucoadhesion time in the range of 24-48hrs., and in-vitro drug release was performed using dynamic Franz Diffusion cell and analyzed using BIT-SOFTWARE. The experimental animals showed improved activity score on actophotometer. The formulated nanosized aripiprazole loaded bio-flexy films showed pharmacotherapeutic response. Conclusion can be drawn that optimized formulation showed effective Pharmacodynamic activity and can be used as for improving therapeutic efficacy of aripiprazole through this platform.
  • Fulminant hepatic failure caused by herbal supplies Article

    Santos Júnior, Genário Oliveira; Ferreira Filho, Raymundo Paraná; Foulon, Liana Machado de Codes; Noblat, Lúcia de Araújo Costa Beisl

    Abstract in English:

    The consumption of botanicals for therapeutic purposes has increased significantly in recent years. Drug-induced liver disease (DILI) is a frequent cause of acute liver injury, around 50% in the United States, and about 1% is secondary to the use of phytotherapeuticals and herbal supplies. Ruellia bahiensis, a plant species of the Acanthaceae family, is a tropical plant distributed in Northeastern Brazil. In folk medicine in the state of Bahia, the species is known as “mãe-boa” and is commonly used. L.S.S, a 23-year old, female, patient was admitted at University Hospital of Bahia-Brazil with signs and symptoms of acute hepatitis. She had made daily use of an herbal supply popularly known as “mãe-boa” for at least two years prescribed by a physician. Diagnostic investigation was negative for viral and autoimmune hepatitis, leptospirosis, dengue, and CMV (cytomegalovirus). The patient had to undergo liver transplantation. Explant revealed massive hepatic necrosis. According to histological findings, and after exclusion of other etiologies, liver damage was assigned to herbal supply. The prolonged use of Ruellia bahiensis infusions may have caused the liver dysfunction.
  • Evaluation of community pharmacists’ involvement in public health activities in Nigeria Article

    Osemene, Kanayo Patrick; Erhun, Wilson Oyekigho

    Abstract in English:

    The aims of the study were to identify the types, determine the extent of community pharmacists’ involvement, and evaluate the factors influencing their participation in public health activities in Nigeria. The study was a cross-sectional survey of randomly selected 130 registered community pharmacies. Pretested questionnaire was the instrument for data collection. Descriptive and inferential statistics were used to analyse data. Response rate was 94.9%. The study identified 31 types of public health activities which community pharmacists participated in. Their extent of involvement was highest in patient counseling (4.93 ± 0.25), personal hygiene (4.90 ± 0.37), maintenance of normal blood pressure (4.88 ± 0.32), and techniques for using vagina pessaries (4.85 ± 0.38). Lowest areas of involvement were elimination of smokeless tobacco use (2.27 ± 1.56), use of seat belts when driving (2.03 ± 1.46), and the need to live in a safe neighborhood (1.42 ± 0.53). Inadequate training (96%), lack of pharmacists’ time (94.6%), inadequate personnel (92.3%), lack of patients’ time (88.5%), lack of profit (85.4%), inadequate space in the pharmacy (82.3%) and inadequate patients’ information (69.9%) significantly influenced their participation. The study concluded that community pharmacists would participate more in public health activities if the identified barriers are reduced.
  • In vitro UV absorption properties and radical scavenging capacity of Morella parvifolia (Benth.) Parra-Os. extracts Article

    Puertas-Mejía, Miguel Angel; Gutierrez-Villegas, María Isabel; Mejía-Giraldo, Juan Camilo; Winkler, Robert; Rojano, Benjamín

    Abstract in English:

    The goal of this research was to identify major compounds of the aerial parts of M. parvifolia (Benth.) Parra-Os., that could enhance its possible application as additive in dermocosmetic products, as well as evaluate the antioxidant properties. The extracts agreed with the broad-spectrum UVB/UVA absorption detected and could act as broad-spectrum sunscreens, covering the UVA and UVB range. Methanolic extracts showed an important antiradical capacity (0.46 and 0.47 g/µmol DPPH), TPC (37.58 and 51.41mg GAE/g DS) and TAC (1.12 and 3.31 mg C3GE/g DS) in fruits and leaves, respectively. M. parvifolia could be considered as a prospective source of natural UV-radiation absorbers with antioxidant capacity. Although the results have clearly demonstrated the potential photoprotection capacity, more studies are needed to enhance its application as an additive in pharmaceutical and medicinal formulations.
  • Demographic, clinical and lifestyle predictors for severity of erectile dysfunction and biomarkers level in Malaysian patients Article

    Mark, Raymond; Huri, Hasniza Zaman; Razack, Azad Hassan Abdul

    Abstract in English:

    The incidence of erectile dysfunction (ED) is rising worldwide and its prevalence is one of the main health concerns that affect overall men well-being in Malaysia. The cluster of demographic, clinical and lifestyle factors may have contributed to the severity of ED and changes in biomarkers level; nevertheless these have not been studied extensively. This cross sectional study involved a total of 276 patients with 138 was diagnosed with ED. The demographic, clinical, lifestyle factors and severity of ED were assessed using a set of questionnaire and the International Index of Erectile Function (IIEF-5). Meanwhile, Total Testosterone (TT) and Asymmetric dimethylarginine (ADMA) levels were determined using the enzyme-linked immunosorbant assay (ELISA). Binary logistic regression test was used to demonstrate the predictors of severity of ED, TT and ADMA levels. Significant predictors for worsening of severity of ED are self-employed [10.55 (0.43 - 257.06), p=0.004], pensioner [8.07 (0.19 - 352.45), p=0.026], non-government employee [1.16 (0.05 - 26.26), p=0.04] and TT [0.41 (0.25 - 0.69), p=0.001]. Nevertheless, pensioner [0.08 (0.01 - 0.87), p=0.038] and unemployed [0.04 (0.01 - 0.42), p=0.007], were the predictors that may influence the changes of TT levels. On the other hand, academic qualification (secondary) [4.51 (0.48 - 42.83), p=0.014] and intensity of physical activities (< 1 hour/day) [2.61 (0.65 - 10.48), p=0.008] were the predictors which were more likely to influence the changes of ADMA levels in ED patients. TT and ADMA levels were influenced by demographic and lifestyle factors whilst severity of ED was predicted by demographic and clinical factors in Malaysian ED population. These predictors may provide new knowledge on risk factors of severity of ED and help in management of ED. Thus, the predictive models could serve as a primary guidance to physicians to ensure ED being managed and treated more effectively.
  • Molecular characterization of Mycobacterium tuberculosis and Mycobacterium bovis isolates by Enterobacterial Repetitive Intergenic Consensus-PCR Article

    Caleffi-Ferracioli, Katiany Rizzieri; Baldin, Vanessa Pietrowski; Noguti, Érika Noda; Siqueira, Vera Lucia Dias; Scodro, Regiane Bertin Lima; Pavan, Fernando Rogério; Hirata, Mario Hiroyuki; Cardoso, Rosilene Fressatti

    Abstract in English:

    Tuberculosis (TB) is an infectious disease in which the molecular typing methods allow to have important information about the dynamics of transmission and to assist properly in disease control. Although the ERIC-PCR (Enterobacterial repetitive intergenic consensus-PCR) assay is fast and easy to perform, scarce studies have reported its use in epidemiological studies in TB outbreaks. In this study, we aimed to genotype Mycobacterium tuberculosis and M. bovis isolates by ERIC-PCR and compare its discriminatory power with two other classically used methods: 12 loci-MIRU (Mycobacterial Interspersed Repetitive Units) and Spoligotyping. The M. tuberculosis isolates studied were from northwestern and southwestern and M. bovis from northwestern Parana, Brazil. ERIC-PCR rendered banding patterns with great diversity (1 to 12 bands) of molecular sizes, ranging from 100 to 1600 bp. ERIC-PCR showed to be fast, simple and affordable to differentiate isolates. ERIC-PCR would be an important tool in the epidemiology of TB as screening in case of outbreak, which demands rapid intervention. However if any doubt persist, as it may occur with the application of only one genotypic method, other genotyping methods should be applied and carefully interpreted, always with additional epidemiological information.
  • Determination of cefotaxime, cefoperazone, ceftazidime and cefadroxil using surface plasmon resonance band of silver nanoparticles Article

    Salem, Hesham; Samir, Ebtihal

    Abstract in English:

    The aim of this work is to evaluate simple, sensitive, effective and validated procedures for the determination of cefotaxime, cefoperazone, ceftazidime and cefadroxil. In this study, the methods based on the ability of the cited drugs to reduce Ag+ ions to silver nanoparticles (Ag-NPs) in the presence of Polyvinyl Pyrrolidone (PVP) as a stabilizing agent producing very intense surface plasmon resonance peak of Ag-NPs (λmax. = 410-430 nm). The plasmon absorbance of the Ag-NPs allows the quantitative spectrophotometric determination of the cited drugs. The calibration curves are linear with concentration ranges of 0.4-3.2, 1-8, 0.5-4.0 and 1.5-9.0 µg/mL for cefotaxime, cefoperazone, ceftazidime and cefadroxil, respectively. Apparent molar absorptivity, detection and quantitative limits are calculated. Applications of the proposed methods to representative pharmaceutical formulations are successfully presented. The extracellular synthesis of nanoparticles is fast, and the method doesn’t require various elaborate treatments and tedious extraction procedures.
  • A novel effect of geraniin on OPG/RANKL signaling in osteoblasts Article

    Zhang, Xiaochao; Yang, Renhua; Long, Jiang; He, Bo; Zhang, Yue; Fu, Ting; Shen, Zhiqiang; Chen, Peng

    Abstract in English:

    In this study, the effects of geraniin on osteoprotegerin/receptor activator of nuclear factor-κB ligand(OPG/RANKL) in regulating the proliferation of osteoblasts and suppression of osteoclast-like cells (OLC) in OLC-osteoblast co-cultured system in vitro were investigated. Osteoblasts were cultured and identified with alkaline phosphatase (ALP), gomori stain, and mineralized nodule stain. OLCs were isolated from long bones of Sprague-Dawley (SD) rats and identified with tartrate-resistant acid phosphatase(TRAP) stain. Methyl thiazolyl tetrazolium assay was used to examine the proliferation of osteoblasts, and immunocytochemistry and in situ hybridization to analyze the expression OPG/RANKL in osteoblasts co-cultured with osteoclasts under the action of geraniin, respectively. Geraniin could regulate the proliferation of osteoblasts MC3T3-E1, decrease the number of OLC in OLC-osteoblast co-cultured system, and inhibit the bone resorption areas and resorption pits of OLC in vitro experiments. Geraniin could promote the mRNA and protein expression levels of OPG and suppress those of RANKL in osteoblasts. These results indicate that geraniin has a promoting effect on the proliferation of osteoblasts and an inhibitory effect on the osteoclastic bone-resorption through regulating OPG/RANKL signaling pathway in OLC-OB co-cultured system.
  • Appraisal of acute oral toxicity of glucuronoxylan hydrogel from Mimosa pudica seeds Article

    Muhammad, Gulzar; Hussain*, Muhammad Ajaz; Ashraf, Muhammad Umer; Naeem-ul-Hassan, Muhammad; Bukhari, Syed Nasir Abbas

    Abstract in English:

    Glucuronoxylan hydrogel (GXH) isolated from M. pudica seeds was assessed for acute toxicology in albino mice that were alienated into four groups. Three groups, i.e., II, III and IV received GXH at a dose of 1, 2 and 5 g/kg, respectively while group I was retained untreated and provided routine diet. After administering GXH, mice were examined for vomiting, diarrhea, allergy and tremors for 8 h. All animals were carefully observed for food and water consumption at 1, 2, 3, 7 and 14 day after administering GXH. At the end of studies, blood samples were drawn for investigation of hematological and biochemical parameters. All animals were sacrificed, relative body weight of vital organs was calculated and their histopathology was studied. It was concluded that there was insignificant difference in body weight, behavioral pattern, food and water intake among treated and control groups. Haematology and biochemistry of blood samples from all groups were found analogous. Histopathological evaluation of vital body organs exhibited no lesions in all groups. Ocular, cardiac and dermal safety of GXH was also established on albino rabbits.
  • Citral effect in male NMRI mice nonalcoholic steatosis model: assessing biochemical and histological parameters and PPARα gene expression Article

    Vaezi, Maryam; Yaghmaei, Parichehreh; Hayati-Roodbari, Nasim; Irani, Shiva; Ebrahim-Habibi, Azadeh

    Abstract in English:

    Citral is a small molecule present in various citrus species, with reported anti-hyperlipidemic and anti-inflammation effects. Here, the effect of intraperitoneal (IP) administration of citral is evaluated in a mouse model of non-alcoholic steatosis. Male NMRI mice were divided into the following groups (n = 12): normal control group (NC) receiving a normal diet; high-fat emulsion group (HF) receiving high fat diet for four weeks; positive control group (C+) receiving HF diet for four weeks and then shifted to normal diet with IP-administered silymarin (80 mg/kg) for four weeks; sham group receiving HF diet for four weeks and then shifted to normal diet for four weeks; and EC1, EC2, and EC3 groups receiving HF diet for four weeks and then shifted to normal diet with IP-administered citral doses of 5, 10, and 20 mg/kg, respectively. HF diet resulted in steatohepatitis with impaired lipid profile, high glucose levels and insulin resistance, impaired liver enzymes, antioxidants, adiponectin and leptin levels, decreased PPARα level, and fibrosis in the liver tissue. Upon treatment with citral, improvement in condition was observed in a dose-dependent manner-both at histological level and in the serum of treated animals. and the PPARα level was also increased.
  • Correlation between rheological properties and capillary fixation for modelling creams Article

    Demoliner, Lara Brogni; Agnol, Lucas Dall; Zanotti, Suzana Bittencourt; Dias, Fernanda Trindade Gonzalez; Angeli, Valeria Weiss; Bianchi, Otavio

    Abstract in English:

    The Brazilian male beauty market occupies the second place in world consumption of cosmetics. Among the numerous products consumed by such audience is the capillary fixation mask, which is mainly composed by fixatives. These additives act on stabilizing the cosmetic emulsion, protecting the hair against moisture and also increasing the intensity of hair fixation. In this work, three formulations for modelling creams were prepared by different concentrations of the fixatives StylezeTM W20 and PVP K90 and their properties characterized by physicochemical, rheological and sensory analysis. The capillary masks produced were stable oil-in-water (O/W) emulsions with uniform droplets of 2.05-2.82 μm sizes and pseudoplastic thixotropic behavior (0.19 < n < 0.26). It was possible to correlate the increased concentration of PVP K90 to a greater thixotropy and an improved yarn fixation, despite the worsening in the spreadability of the formulations. These results suggest properly conducted rheological measurements can contribute to the prediction of the emulsion’s sensory properties, which can save time and funds on the development of new cosmetics.
  • Comparative evaluation of pancreatic histopathology of rats treated with olanzapine, risperidone and streptozocin Article

    Shah, Rehmat; Subhan, Fazal; Sultan, Sayed Mohammad; Ali, Gowhar; Ullah, Ihsan; Ullah, Sami

    Abstract in English:

    Olanzapine and risperidone are widely prescribed atypical antipsychotics used in the treatment of schizophrenia and various other psychiatric disorders. Both of these drugs have been extensively reported to cause Type 2 diabetes mellitus and pancreatitis, however, the mechanism of olanzapine and risperidone-induced toxicity has not been so far unveiled. We, therefore, compared the streptozocin-induced pancreatic damage with that of pancreas isolated from olanzapine and risperidone treated rats. It was noticed that fibrotic growth, necrosis and derangement of the pancreatic islet cells caused by streptozocin were more pronounced than olanzapine and risperidone.
  • Beta-glucan prevents toxic effects of 2,3,7,8-TCDD in terms of oxidative and histopathological damage in heart tissue of rats Article

    Ciftci, Osman; Duman, Ahmet Sefa; Turkmen, Neşe Basak; Taslıdere, Aslı

    Abstract in English:

    2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) is a widespread environmental contaminant which causes severe toxic effects. Despite there is some suggestion concerning with TCDD induced cardiotoxicity such as formation of free radicals, the main mechanism has not been entirely explained. Beta-glucan is known as strong antioxidant matter and can scavenge free radicals. Therefore this study aimed to investigate the protective effects of beta-glucan against TCDD induced cardiotoxicity in rats. In this study, 2-3 months of age and 190-250 g in weight 32 rats were randomly divided into four equal groups (n=8 for each group). Group 1 was control; Group 2 was TCDD group (2 µg/kg/week); group 3 was the beta-glucan group(50 mg/kg/day), and group 4 was TCDD and beta-glucan treatment group. The heart samples were taken from rats after 21 days treatment. The results were shown that Despite TCDD exposure visibly caused to increase (p ≤ 0.001) in TBARS levels, It caused a visible decline in the levels of GSH, CAT, GSH-Px, and SOD. However Beta glucan significantly increased GSH, CAT, GSH-Px, SOD levels and decreased generation of TBARS. Additionally, our histopathological observations were in agreement with the biochemical results. In conclusion, Beta-glucan treatment exhibited protective activity on TCDD induced cardiotoxicity.
  • Stability and in vivo efficiency of natural cosmetic emulsion systems with the addition of vegetable oils Article

    Pavlačková, Jana; Kovacsová, Klára; Radiměřský, Petr; Egner, Pavlína; Sedlaříková, Jana; Mokrejš, Pavel

    Abstract in English:

    The aim of the paper is to test stability and biophysical properties of hydrophilic and lipophilic emulsions with selected vegetable seed oils: Limnanthes alba, Prunus amygdalus dulcis, Cannabis sativa, Rosa rubiginosa and Hellianthus annuus. Biophysical properties of emulsions are investigated in vivo using non-invasive instrumental methods (corneometry, tewametry and pH) in a group of 12 healthy women volunteers. Their stability profiles (colour, phase separation and centrifugation) under various temperatures (9, 25, 37 and 57 °C) and storage time (24 hours, 2, 7, 14, 21 and 28 days) were monitored. The moisturising activities of the emulsions supplemented with various oils were comparable. The lipophilic emulsions showed a better ability to improve the condition of the skin barrier due to formation of a surface lipid film. The tested formulations regulated the pH of the skin towards neutral values. Lipophilic emulsions showed earlier phase separation and changes in colour. The greatest resistance to thermal stress during storage was observed for the emulsion bases. Emulsions containing oils, except for those with rosehip and hempseed oils, were stable up to the temperature of 37 °C. The studied emulsion systems are excellent vehicles of vegetable oils and exhibit relatively good stability, benefiting the natural properties of skin.
  • Hepatoprotective effect of Alhagi sparsifolia against Alcoholic Liver injury in mice Article

    Maimaitimin, Kuerbanjiang; Jiang, Zhihui; Aierken, Aili; Shayibuzhati, Mikeremu; Zhang, Xiaoying

    Abstract in English:

    Overconsumption of alcohol leads to alcoholic liver disease (ALD). Natural compounds have been investigated previously for their hepatoprotective activities against liver injury. This study investigated the protective effect of Alhagi sparsifolia on ALD. Alcohol was administered to mice for three consecutive days; either alone or in combination with Alhagi sparsifolia extract (150, 300, 600 mg/kg). Serum aspartate aminotransferase and alanine transaminase as biomarkers of liver injury, the content of malonaldehyde, hydrogen peroxide (H2O2) and glutathione which indicated the redox status of liver and the antioxidant enzyme activity of super oxide dismutase were detected, respectively. Moreover, the expression of protein cytochrome P450 2E1 (CYP2E1) the key enzyme of alcohol metabolism, and also tested by western blot experiment. Subsequently, the mRNA levels of inflammatory factors including TNF- α and TLR4 was determined real-time PCR. Results showed that Alhagi sparsifolia significantly alleviated alcohol-induced liver injury by reducing serum ALT and AST, inhibiting MDA and H2O2 content, increasing SOD, and GSH level in the liver (P< 0.05). In addition, the Alhagi sparsifolia treatment inhibited the expression of CYP2E1 (P< 0.05). The results suggest that Alhagi sparsifolia could be a promising natural substance for ameliorating acute alcohol-induced oxidative stress and hepatic injury.
  • Therapeutic itinerary: trajectory for resolution of adverse events of patients using warfarin in Southern Brazil Article

    Colet, Christiane; Amador, Tânia Alves; Heineck, Isabela

    Abstract in English:

    Warfarin is the most used anticoagulant in primary health care. Due to the narrow therapeutic index, its users are more susceptible to adverse events. The objective of this study was to describe the itinerary of the public health sector patients for resolution of adverse events related to warfarin. It is a prospective open cohort, held for a period of 18 months with warfarin users of the Brazilian public health system. Data were collected by monthly interviews and from patient records. Results: Sixty nine patients were interviewed, 64 of them completed monitoring and five died. Bleeding and venous thromboembolism were more frequent in patients starting treatment. It was observed that when adverse events have occurred, in most cases the patient held self-care at home (57%). During the follow-up, five patients were hospitalized for bleeding. Approximately half of the patients did not present their INR exams to the doctor. Conclusions: This study demonstrates weaknesses in caring for these patients and the need to accompany them, aiming to standardize and guide the itinerary of the anticoagulated patient to solve their problems and improve safety in drug treatment, with less cost to the public health system.
  • Protective effect of luteolin on the transgenic Drosophila model of Parkinson’s disease Article

    Siddique, Yasir Hasan; Jyoti, Smita; Naz, Falaq; , Rahul

    Abstract in English:

    In the present study we have studied the effect of 25, 50, 75 and 100 µM of luteolin on the transgenic Drosophila expressing human alpha synuclein. The doses of luteolin were established in diet and the PD flies were allowed to feed on it for 24 days. After 24 days of exposure the flies were assayed for climbing assay, oxidative stress markers, caspase-3 & 9 activity and dopamine content. The immunohistochemistry was also performed on the brain sections for the activity of tyrosine hydroxylase. The exposure of luteolin showed a dose dependent delay in the loss of climbing ability and activity, reduction in oxidative stress markers, caspase-3&9 activities and results in an increase in the dopamine content. The results obtained for the immunohistochemistry also supports the protective role of luteolin against the damage of the dopaminergic neurons.
  • Effects of Cinnamomum cassia extract on oxidative stress, immunreactivity of iNOS and impaired thoracic aortic reactivity induced by type II diabetes in rats Article

    Uslu, Gözde Atila; Gelen, Volkan; Uslu, Hamit; Özen, Hasan

    Abstract in English:

    Type II diabetes is known to cause neuropathy, nephropathy and retinopathy. However, cardiovascular disorders associated with diabetes have been ignored. In traditional medicine, cinnamon (Cinnamomum cassia) bark has been used for its abilities to relieve fever, inflammation and chronic bronchitis. In the present study, the effect of Cinnamomum cassia extract (CN) on the thoracic aorta in an experimental type II diabetes model was investigated. In rats administered with nicotinamide + streptozotocin, significant endothelial dysfunction and oxidative stress were characterised by increased inducible nitric oxide synthase (iNOS) and decreased insulin/proinsulin levels. This impairment was prevented by administering 1000 mg/kg metformin or 500-1000-1500 mg/kg CN. CN administration attenuated the inflammatory response by decreasing the levels of malondialdehyde (MDA), Nitric oxide (NO) and increasing Glutathione peroxidase (GPx), glutathione (GSH). In addition, CN administration was shown to cause down-regulating effects on iNOS in thoracic aorta. These findings reveal that CN could prevent chronic complications of experimentally induced type II diabetes by attenuating inflammation, oxidant/antioxidant imbalance, and normalised contraction and relaxion responses in the thoracic aorta.
  • Cytotoxic and apoptotic potential of Myristica fragrans Houtt. (mace) extract on human oral epidermal carcinoma KB cell lines Article

    Rengasamy, Gayathri; Venkataraman, Anuradha; Veeraraghavan, Vishnu Priya; Jainu, Mallika

    Abstract in English:

    Several studies have revealed that certain naturally occurring medicinal plants inhibit the growth of various cancers. The present study was conducted to evaluate cytotoxicity and apoptotic induction potential of Myristica fragrans Houtt mace extract. The cytotoxic activity of the Myristica fragrans Houtt mace acetone extract was assayed by MTT assay on human oral epidermal carcinoma KB cell lines. KB cells were incubated with different concentration of mace extract ranging from 25 to 125 μg/mL for 24hrs. The apoptotic induction potential was also studied by the analysis of Bcl-2 protein and gene expression in mace extract incubated KB cell lines using western blotting technique and real-time polymerase chain reaction. The mace extract exhibited cytotoxicity and anticancer effect against KB cell lines and it also suppressed the growth of cancer cells, therefore growth inhibitory effect was noted in extract treated cell lines. The apoptotic potential of mace extract was accompanied by reduced gene expression of Bcl-2 compared to the untreated KB cells. The mace extract shows the cytotoxic activity and induced the apoptosis through the modulation of its target genes Bcl-2 in the KB cell lines, suggesting the potential of mace as a candidate for oral cancer chemoprevention. This can be further investigated in vivo for its anticancer potential.
  • Hypoglycemic activity of Capparis ovata desf. var. palaestina zoh. methanol extract Article

    Okur, Mehmet Evren; Özbek, Hanefi; Polat, Derya Çiçek; Yılmaz, Sezen; Arslan, Rana

    Abstract in English:

    Caper (Capparis ovata Desf. and Capparis spinosa L.) is naturally widespread in Turkey. Traditionally, buds, fruits, seeds and roots of this plant are used as tonic, diuretic, anti-rheumatic, expectorant, antidiabetic, and antifungal. The aim of this study is to evaluate potential hypoglycemic effect of C. ovata var. palaestina extracts in alloxan-induced diabetic mice. For this purpose; diabetic mice were administered with 100, 300, 500 mg/kg (i.p.) doses of methanol extract of bud and fruit. Blood glucose levels were screened 60, 120, 240 and 360 min. after treatment. Furthermore, high resolution mass spectrometry (HRMS) analysis, ABTS and DPPH free radical scavenging activity test, and phenolic and flavonoid compounds analysis of extracts were carried out. The data obtained from in vivo study revealed that fruit-methanol 500 mg/kg (FM3), bud-methanol 300 mg/kg (BM2), bud-methanol 500 mg/kg (BM3) extracts showed significant hypoglycemic activity. All extracts indicated significant antioxidant activity, however bud-methanol (BM) extract demonstrated the most potent antioxidant activity. Moreover high levels of phenolic substances and flavonoids were involved in all extracts, but the highest levels were found in FM extract. HRMS study showed that rutin, quercetin 3-O-glucoside (isoquercitrin) and stachydrine substances had seen in BM extract. The results of this study showed that the C. ovata var. palaestina extracts which, indicate hypoglycemic, antioxidant activities, might provide additional support in diabetes.
  • Determination of phytoconstituents of n-hexane extract of leaves of Morus nigra and evaluation of their effects on biochemical and histopathological parameters in paracetamol intoxicated mice liver Article

    Mallhi, Tauqeer Hussain; Qadir, Muhammad Imran; Khan, Yusra Habib

    Abstract in English:

    In-vitro investigation of Morus nigra L. (Moraceae) has demonstrated the evidence of several antioxidant compounds. Current study was aimed to determine the phytoconstituents and hepatoprotective potential of n-hexane extract of Morus nigra. Swiss albino mice were divided into five groups: normal control, paracetamol control, silymarin control, 250 mg/kg p.o. extract for 7 days plus paracetamol 3 h later, 500 mg/kg p.o. extract for 7 days plus paracetamol 3 h later. Serum levels of liver enzymes and total bilirubin were assessed and compared between the groups by using one-way ANOVA to confirm hepatoprotective activity. HPLC analysis revealed the presence quercetin, oleanolic acid, luteolin, apigenin, vitamin C and kuwanon C. n-hexane extract of Morus nigra at dose of 250 mg/kg reduced elevated ALT by 54.3% (p<0.001), AST by 55.1% (p<0.01), ALP by 28.5% (p<0.01) and TBR by 56.4% (p<0.01) as compared to paracetamol control. The dose of 500 mg/kg of the extract reduced the ALT levels by 62.9% (p<0.001), AST by 56.7% (p<0.01), ALP by 33.6% (p<0.01) and TBR by 54.5% (p<0.01), as compared to paracetamol group. However, the reduction of liver enzymes and total bilirubin after administration of extract was comparable to the silymarin. Current study demonstrated potential hepatoprotective activity of n-hexane extract of Morus nigra.
  • Erratum: Fast detection of Mycobacterium tuberculosis in culture-positive sputum samples by nitrate reductase activity Erratum

Universidade de São Paulo, Faculdade de Ciências Farmacêuticas Av. Prof. Lineu Prestes, n. 580, 05508-000 S. Paulo/SP Brasil, Tel.: (55 11) 3091-3824 - São Paulo - SP - Brazil
E-mail: bjps@usp.br